Advanced Science, EarlyView.Lysosome‐targeting chimeras (LYTACs) enable degradation of extracellular and membrane proteins via lysosomal trafficking. We report a novel IGF‐II mutant (Del1–7, Y27L) that selectively engages IGF‐IIR while avoiding IGF‐IR and IR‐A. mutIGF‐II–based LYTACs enhance target internalization and degradation and support a genetically encodable, all‐protein ...
Yuan Zhao +16 more
wiley +1 more source
Specificity for deubiquitination of monoubiquitinated FANCD2 is driven by the N-terminus of USP1 [PDF]
, 2018 The Fanconi anemia pathway for DNA interstrand crosslink repair and the translesion synthesis pathway for DNA damage tolerance both require cycles of monoubiquitination and deubiquitination.
Arkinson, Connor +3 more
core +3 more sources
PSMA8‐Containing 20S Proteasome Regulates Spermiogenesis and Male Fertility
Advanced Science, EarlyView.PSMA8 assembles s20S proteasome that degrades specific substrates in elongating spermatids. Degradation of s20S‐substrates activates translation of FXR1‐target mRNAs, which are essential for mitochondrial sheath formation and sperm morphogenesis.
Huiwen Cao +7 more
wiley +1 more source
PTGES3 proteolysis using the liposomal peptide-PROTAC approach
Biology DirectBackground Hepatocellular carcinoma (HCC) is the leading cause of cancer-related deaths worldwide, and the lack of effective biomarkers for early detection leads to poor therapeutic outcomes.
Shiwei Liu +6 more
doaj +1 more source
Design and applications of bifunctional small molecules: Why two heads are better than one [PDF]
, 2008 Induction of protein−protein interactions is a daunting challenge, but recent studies show promise for small molecules that specifically bring two or more protein molecules together for enhanced or novel biological effect.
Aberle, Nicholas +2 more
core +1 more source
Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras [PDF]
ACS Central Science, 2016 Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a promising potential alternative to protein inhibition for therapeutic intervention. Current PROTAC molecules incorporate a ligand for the target protein, a linker, and an E3 ubiquitin ligase recruiting group, which bring together target protein and ubiquitinating ...
Honorine Lebraud +3 more
openaire +3 more sources
Leveraging Macrophage Metabolic Reprogramming for Enhanced Anti‐Tumor Immunity
Advanced Science, EarlyView.Tumor‐associated macrophages (TAMs) are key regulators of the tumor microenvironment (TME), with their metabolic states playing a critical role in tumor progression or regression. This review summarizes current understanding of TAM metabolic plasticity alongside cutting‐edge bioengineering innovations, outlining a roadmap for transforming the ...
Zhiyun Liu +8 more
wiley +1 more source
Galectins as New Prognostic Markers and Potential Therapeutic Targets for Advanced Prostate Cancers [PDF]
, 2013 A better understanding of multimolecular interactions involved in tumor dissemination is required to identify new effective therapies for advanced prostate cancer (PCa).
Compagno, Daniel Georges +3 more
core +3 more sources
IRT5 Probiotics Changes Immune Modulatory Protein Expression in the Extraorbital Lacrimal Glands of an Autoimmune Dry Eye Mouse Model [PDF]
, 2020 PURPOSE. While the association between the gut microbiome and the immune system has been studied in autoimmune disorders, little is known about ocular disease.
Choi, Se Hyun +6 more
core +1 more source
First Generation Proteolysis Targeting Chimeras (PROTACs) for the Treatment of Progeria
Advanced Science, EarlyView.We report the first PROTACs designed to degrade progerin, introducing a novel therapeutic approach for progeria. The best compound, UCM‐18142, significantly reduces progerin levels and improves key disease phenotypes in patient‐derived cells and in the LmnaG609G/G609G mouse model, paving the way for new treatment strategies targeting the root cause of ...
Jon Macicior‐Michelena +5 more
wiley +1 more source